FIELD: organic chemistry, biochemistry, medicine, oncology. SUBSTANCE: invention relates to novel derivatives of imidazole of the formulas (I) and (II) wherein l, m, r, s and t = 0 or 1; n = 1 or 2 under condition that when l and m = 0 then n = 2; Y means SO2 or CH2; Z means CR12,NR32SO2,NR13,NR36CO,OCONR15,SO2NR14; R1 is taken among the group consisting of hydrogen atom, alkyl or aralkyl and symbol means a simple or double bond; R7,R8 are taken among the group consisting of hydrogen atom, aryl, -CN, halide and U-R44 where U means oxygen atom; R44 and R11 are taken among the group consisting of hydrogen atom, alkyl, aralkyl, aryl; R32 is taken among the group consisting of hydrogen atom, unsubstituted lower alkyl or lower alkyl substituted with phenyl and thienyl; R9,R10,R12,R13,R14,R15,R36,R37,R38 represent hydrogen atom or lower alkyl; one of R, S and T represents CH2 or CH(CH2)pQ where Q means NR57R58 wherein p = 0, 1 or 2 under condition that when Y means SO2 then R11 can not mean hydrogen atom. Invention relates also to its enantiomers, diastereomers, pharmaceutically acceptable salts and solvates. Invention relates also to pharmaceutical composition based on these compounds, methods for inhibition of activity of farnesyl protein transferase and prenyltranseferase and inhibition of the tumor growth. Invention provides preparing novel derivatives of imidazole eliciting inhibitory activity with respect to farnesyl protein transferase and prenyl- transferase and usable for suppression of growth of tumors. EFFECT: improved inhibition methods, valuable medicinal properties of compounds. 14 cl, 1 tbl, 30 ex
Title | Year | Author | Number |
---|---|---|---|
DERIVATIVES OF IMIDAZOLE | 1997 |
|
RU2225405C2 |
SYNERGIC METHODS AND COMPOSITIONS FOR CANCER TREATMENT | 2001 |
|
RU2264217C2 |
BENZOTHIAZOLE INHIBITORS OF PROTEIN TYROSINE KINASES | 1998 |
|
RU2212407C2 |
COMPLEX OF RAS-FARNESYLTRANSFERASE INHIBITOR, COMPOSITION OF RAS-FARNESYLT RANSFERASE INHIBITOR, PHARMACEUTICAL COMPOSITION | 1999 |
|
RU2230062C2 |
AMINOTHIAZOLE INHIBITORS OF CYCLIN-DEPENDENT KINASES | 1998 |
|
RU2211839C2 |
PYRROLTRIAZINE KINASE INHIBITORS | 2000 |
|
RU2331640C2 |
METHOD FOR TREATMENT OF STATES CAUSED BY p38 KINASES AND PYRROLOTRIAZINE COMPOUNDS USED AS KINASE INHIBITORS | 2001 |
|
RU2316556C2 |
HETEROCYCLIC DIHYDROPYRIMIDINE COMPOUNDS | 2000 |
|
RU2296766C2 |
NEW KINASE INHIBITORS | 2003 |
|
RU2331642C2 |
CYCLIC INHIBITORS OF PROTEIN-TYROSINE KINASE | 2000 |
|
RU2312860C2 |
Authors
Dates
2003-09-10—Published
1998-06-16—Filed